[go: up one dir, main page]

PE20080316A1 - AZIRIDINYL-EPOTILONE COMPOUNDS - Google Patents

AZIRIDINYL-EPOTILONE COMPOUNDS

Info

Publication number
PE20080316A1
PE20080316A1 PE2007000648A PE2007000648A PE20080316A1 PE 20080316 A1 PE20080316 A1 PE 20080316A1 PE 2007000648 A PE2007000648 A PE 2007000648A PE 2007000648 A PE2007000648 A PE 2007000648A PE 20080316 A1 PE20080316 A1 PE 20080316A1
Authority
PE
Peru
Prior art keywords
rent
epotilone
aziridinyl
compounds
substitute
Prior art date
Application number
PE2007000648A
Other languages
Spanish (es)
Inventor
Gregory D Vite
Soong-Hoon Kim
Christopher P Leamon
Iontcho Vlahov
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20080316A1 publication Critical patent/PE20080316A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/396Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having three-membered rings, e.g. aziridine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/551Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

REFERIDA A UN COMPUESTO AZIRIDINIL-EPOTILONA DE FORMULA (X), DONDE K ES O, S O NR7; A ES -(CR8R9)-(CH2)m-Z-; Z ES (CHR10), C(=O), -OC(=O), ENTRE OTROS; B1 ES OH O CIANO Y R1 ES HIDROGENO O B1 Y R1 JUNTOS FORMAN UN ENLACE DOBLE; R2, R3 Y R5 SON H, ALQUILO, ARILO, ENTRE OTROS; R4 ES H, ALQUILO, ALQUENILO, ENTRE OTROS; R6 ES H, ALQUILO O ALQUILO SUSTITUIDO; R12 ES H, ALQUILO, ALQUILO SUSTITUIDO O HALOGENO; R13 ES ARILO, HETEROARILO, ENTRE OTROS; m ES UN ENTERO DE 0 A 6. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE CANCERES, EN ESPECIAL AQUELLOS RELACIONADOS CON LA EXPRESION DEL RECEPTOR DE FOLATOREFERRING TO AN AZIRIDINYL-EPOTILONE COMPOUND OF FORMULA (X), WHERE K IS O, S OR NR7; A ES - (CR8R9) - (CH2) m-Z-; Z IS (CHR10), C (= O), -OC (= O), AMONG OTHERS; B1 IS OH OR CYANE AND R1 IS HYDROGEN OR B1 AND R1 TOGETHER FORM A DOUBLE BOND; R2, R3 AND R5 ARE H, ALKYL, ARYL, AMONG OTHERS; R4 IS H, ALKYL, ALKENYL, AMONG OTHERS; R6 IS H, RENT OR SUBSTITUTE RENT; R12 IS H, RENT, SUBSTITUTE RENT, OR HALOGEN; R13 IS ARYLUS, HETEROARYL, AMONG OTHERS; m IS AN INTEGER FROM 0 TO 6. IT IS ALSO REFERRED TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE USEFUL IN THE TREATMENT OF CANCERS, ESPECIALLY THOSE RELATED TO THE EXPRESSION OF THE FOLATE RECEIVER

PE2007000648A 2006-05-25 2007-05-24 AZIRIDINYL-EPOTILONE COMPOUNDS PE20080316A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US80836606P 2006-05-25 2006-05-25

Publications (1)

Publication Number Publication Date
PE20080316A1 true PE20080316A1 (en) 2008-04-10

Family

ID=38561739

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000648A PE20080316A1 (en) 2006-05-25 2007-05-24 AZIRIDINYL-EPOTILONE COMPOUNDS

Country Status (20)

Country Link
US (2) US7872145B2 (en)
EP (1) EP2041140B1 (en)
JP (1) JP5249929B2 (en)
KR (1) KR101413955B1 (en)
CN (1) CN101495482B (en)
AR (1) AR061181A1 (en)
AT (1) ATE524477T1 (en)
AU (1) AU2007267535B2 (en)
BR (1) BRPI0712167A2 (en)
CA (1) CA2655668C (en)
EA (1) EA014872B1 (en)
ES (1) ES2371111T3 (en)
IL (1) IL195236A (en)
MX (1) MX2008014735A (en)
NO (1) NO20084742L (en)
NZ (1) NZ572763A (en)
PE (1) PE20080316A1 (en)
TW (1) TWI383985B (en)
WO (1) WO2007140297A2 (en)
ZA (1) ZA200810022B (en)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010528115A (en) 2007-05-25 2010-08-19 ブリストル−マイヤーズ スクイブ カンパニー Epothilone compound and method for producing analog
CA2799202C (en) 2010-05-18 2016-07-05 Cerulean Pharma Inc. Compositions and methods for treatment of autoimmune and other diseases
MX371403B (en) 2014-03-20 2020-01-29 Bristol Myers Squibb Co Stabilized fibronectin based scaffold molecules.
CA2968382A1 (en) 2014-11-21 2016-05-26 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
SMT202000413T1 (en) 2014-11-21 2020-09-10 Bristol Myers Squibb Co Antibodies against cd73 and uses thereof
SG11201703760WA (en) 2014-11-25 2017-06-29 Bristol Myers Squibb Co Novel pd-l1 binding polypeptides for imaging
JP2018510864A (en) 2015-03-10 2018-04-19 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Antibody capable of binding by transglutaminase and conjugate produced thereby
CN108137687B (en) 2015-05-29 2021-10-29 百时美施贵宝公司 Anti-OX40 antibody and its use
US10584160B2 (en) 2015-09-23 2020-03-10 Bristol-Myers Squibb Company Glypican-3-binding fibronectin based scaffold molecules
AU2016340093A1 (en) * 2015-10-16 2018-05-10 William Marsh Rice University Epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates thereof
KR20180089433A (en) 2015-12-21 2018-08-08 브리스톨-마이어스 스큅 컴퍼니 Variant antibodies for site-specific conjugation
SG10201913033UA (en) 2016-03-04 2020-03-30 Bristol Myers Squibb Co Combination therapy with anti-cd73 antibodies
WO2018048975A1 (en) 2016-09-09 2018-03-15 Bristol-Myers Squibb Company Use of an anti-pd-1 antibody in combination with an anti-mesothelin antibody in cancer treatment
KR102085798B1 (en) 2016-12-28 2020-03-06 주식회사 인투셀 Compounds comprising beta-galactoside self-immolative linker
CN116333129A (en) 2017-05-25 2023-06-27 百时美施贵宝公司 Antibodies comprising modified heavy chain constant regions
US20220106400A1 (en) 2018-11-28 2022-04-07 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
CN113453725A (en) 2018-11-30 2021-09-28 百时美施贵宝公司 Antibodies comprising glutamine-containing light chain C-terminal extensions, conjugates thereof, and methods and uses
CN113544155A (en) 2018-12-12 2021-10-22 百时美施贵宝公司 Antibodies modified for transglutaminase conjugation, conjugates thereof, and methods and uses
CN110563730B (en) * 2019-07-29 2022-03-25 江苏理工学院 High purity N10Preparation method of (E) -trifluoroacetyl pteroic acid
WO2021055306A1 (en) 2019-09-16 2021-03-25 Bristol-Myers Squibb Company Dual capture method for analysis of antibody-drug conjugates
EP4178982A1 (en) 2020-07-13 2023-05-17 Precirix N.V. Antibody fragment against folr1
EP4079327A1 (en) * 2021-04-22 2022-10-26 Centaurus Polytherapeutics Payloads for drug-conjugates and their use for treating cancer
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
EP4518911A1 (en) 2022-05-02 2025-03-12 Precirix N.V. Pre-targeting

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5108921A (en) 1989-04-03 1992-04-28 Purdue Research Foundation Method for enhanced transmembrane transport of exogenous molecules
US6291673B1 (en) 1997-10-17 2001-09-18 Purdue Research Foundation Folic acid derivatives
US6380395B1 (en) * 1998-04-21 2002-04-30 Bristol-Myers Squibb Company 12, 13-cyclopropane epothilone derivatives
US6291684B1 (en) 1999-03-29 2001-09-18 Bristol-Myers Squibb Company Process for the preparation of aziridinyl epothilones from oxiranyl epothilones
AUPQ014799A0 (en) 1999-05-04 1999-05-27 Access Pharmaceuticals Australia Pty Limited Amplification of folate-mediated targeting to tumor cells using polymers
US6800653B2 (en) 2001-06-01 2004-10-05 Bristol-Myers Squibb Compnay Epothilone derivatives
EP1524979A2 (en) 2002-07-31 2005-04-27 Schering AG New effector conjugates, process for their production and their pharmaceutical use
EP1572242B1 (en) 2002-12-13 2014-04-16 Immunomedics, Inc. Immunoconjugates with an intracellularly-cleavable linkage
TWI405573B (en) * 2003-01-27 2013-08-21 Endocyte Inc Vitamin-receptor binding drug delivery conjugates intermediates and preparation processes
DE602005003453T2 (en) 2004-01-30 2008-09-25 Bayer Schering Pharma Aktiengesellschaft NEW EFFECTOR CONJUGATES, PROCESS FOR THEIR MANUFACTURE AND THEIR PHARMACEUTICAL USE
CN101438252A (en) 2004-10-07 2009-05-20 爱莫里大学 Multifunctional nanoparticle conjugates and their use

Also Published As

Publication number Publication date
CN101495482B (en) 2012-05-02
TW200815452A (en) 2008-04-01
WO2007140297A3 (en) 2008-01-31
CN101495482A (en) 2009-07-29
IL195236A0 (en) 2009-08-03
EP2041140B1 (en) 2011-09-14
US7872145B2 (en) 2011-01-18
JP2009538349A (en) 2009-11-05
EA200802389A1 (en) 2009-06-30
AU2007267535B2 (en) 2012-07-05
AU2007267535A8 (en) 2011-06-09
KR101413955B1 (en) 2014-07-01
CA2655668A1 (en) 2007-12-06
HK1124335A1 (en) 2009-07-10
NZ572763A (en) 2010-08-27
US20070276018A1 (en) 2007-11-29
ZA200810022B (en) 2011-05-25
AU2007267535A1 (en) 2007-12-06
BRPI0712167A2 (en) 2012-08-28
IL195236A (en) 2012-12-31
USRE42930E1 (en) 2011-11-15
CA2655668C (en) 2013-02-26
ES2371111T3 (en) 2011-12-27
AR061181A1 (en) 2008-08-13
JP5249929B2 (en) 2013-07-31
NO20084742L (en) 2008-12-16
EP2041140A2 (en) 2009-04-01
EA014872B1 (en) 2011-02-28
TWI383985B (en) 2013-02-01
ATE524477T1 (en) 2011-09-15
MX2008014735A (en) 2009-02-12
WO2007140297A2 (en) 2007-12-06
KR20090025266A (en) 2009-03-10

Similar Documents

Publication Publication Date Title
PE20080316A1 (en) AZIRIDINYL-EPOTILONE COMPOUNDS
PE20140961A1 (en) MACROCYCLIC INHIBITORS OF SERINE PROTEASES OF HEPATITIS C
PE20080102A1 (en) AZIRIDINYL-EPOTILONE CONJUGATES AND PHARMACEUTICAL COMPOSITIONS INCLUDING THE SAME
MXPA05011166A (en) Cgrp receptor antagonists.
CO6160237A2 (en) PIRAZINONAS AND PIRAZINOLES REPLACED AND COMPOSITIONS THAT INCLUDE THEM
CR20140316A (en) DERIVATIVES OF INDOL AS RECEIVING ANTAGONISTS OF S1P1 (DIVISIONAL 10922)
ATE429427T1 (en) PYRIMIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
EA200702497A1 (en) SUBSTITUTED Arylpyrazoles for use against parasites
RU2010102229A (en) Benzazepine derivatives suitable for use as antagonists of vasopressin
IL182317A0 (en) Cgrp receptor antagonists
MXPA05010824A (en) Bicyclic compounds as nr2b receptor antagonists.
GT200500101A (en) METHYL-ARIL OR HETEROARIL-AMIDA SUBSTITUTED COMPOUNDS
SG162805A1 (en) Pyrazine derivatives useful as adenosine receptor antagonists
ATE466860T1 (en) CGRP RECEPTOR ANTAGONISTS
PE20090042A1 (en) CYCLOPAMINE ANALOGS
MA28550B1 (en) COMPOUNDS AND METHODS FOR TREATING DYSLIPIDEMIA
TW200519096A (en) Quinazoline analogs as receptor tyrosine kinase inhibitors
MY147400A (en) Heterocyclic compounds as ccr2b antagonists
PE20060625A1 (en) BENZAZEPINE DERIVATIVES AS ANTAGONISTS AND / OR AGONISTS OF THE HISTAMINE H3 RECEPTOR
TW200510427A (en) Novel fused heterocycles and uses thereof
EP1804919A4 (en) CGRP RECEPTOR ANTAGONISTS
IL178839A0 (en) Heterocyclic condensed compounds useful as antidiuretic agents
EA200500899A1 (en) ANTAGONISTS OF ADDROSE DIPHOSPHATE PLATELET RECEPTOR
GB0507601D0 (en) Compounds
PE20050336A1 (en) TRICYCLIC COMPOUNDS AS INHIBITORS OF PROTEIN FARNESIL TRANSFERASE

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed